Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists |
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| Authors: | Balavoine Fabrice Malabre Patrice Alleaume Thierry Rey Astrid Cherfils Valérie Jeanneton Olivier Seigneurin-Venin Sophie Revah Frédéric |
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| Affiliation: | Cerep, 19 avenue du Québec Courtaboeuf 1, 91951 Villebon sur Yvette, France. fabrice.balavoine@quantum-genomics.com |
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| Abstract: | We report here new chemical series acting as antagonists of melanin-concentrating hormone receptor 1 (MCHR-1). Synthesis and structure-activity relationships are described leading to the identification of compounds with optimized in vitro pharmacological and in vitro ADME profiles. In vivo activity has been demonstrated in animal models of food intake and depression. |
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